Calcium Channel Blockers (CCB)

  1. Nifedipine (N)
  2. Amlodipine (A)
  3. Diltiazem (D)
  • Bioavailability: nifedipine = 50-70%; diltiazem 20-40%; amlodipine 50-88%
  • Half-life nifedipine and diltiazem = 4h; amlodipine = 35h
  • Protein bound 
  • Excretion: kidney for nifedipine & amlodipine; feces for diltiazem
  • Pregnancy Category C

  • Oral

  • Nifedipine: 30-90 mg daily (extended release)
  • Amlodipine: 5-10 mg daily
  • Diltiazem: 60-120 mg three times a day

  • Inhibits calcium transportation to smooth muscle cells = inhibition of muscle vasoconstriction
  • Also effect on atrioventricular conduction & heart rate
  • Nifedipine: also, synergistic effect on platelet’s anti-aggregation activity

Off label

  • Raynaud phenomenon (Nifedipine; Diltiazem; Amlodipine), primary and secondary
  • Chilblains
  • Calcinosis cutis (especially in systemic sclerosis) (Diltiazem)
  • Wound healing (Nifedipine; Amlodipine)
  • Keloids / hypertrophic scarring (verapamil)
  • Cyclosporine-induced hypertension (Nifedipine)
  • Leiomyoma-associated pain
  • Anal fissures (oral & topical Nifedipine & Diltiazem)

  • Hypersensitivity
  • Precaution with cardiovascular diseases: ischemia, valvular, arrhythmias, etc.

  • Frequent but rarely require discontinuation of treatment
  • * Amlodipine & Diltiazem less severe side effects than Nifedipine
  • Secondary to vasodilatation: peripheral edema (most common, 2-3 weeks after beginning treatment), dizziness, headache (very common), nausea, rarely symptomatic hypotension.
  • Reversible transaminitis (Diltiazem)
  • Mucocutaneous:
    • Gingival hyperplasia (especially with Diltiazem, Nifedipine)
    • Telangiectasia (face / trunk)
    • Psoriasis (exacerbation / new onset)
    • Chronic eczematous reaction in elderly
    • Subacute cutaneous lupus erythematosus
    • Photosensitivity
    • Gynecomastia
    • Erythromelalgia 
    • Oral ulcers
    • Erythema multiforme; Steven-Johnson syndrome / toxic epidermal necrolysis (associated with Diltiazem)

  • Nifedipine: substrate CYP3A4 
  • Amlodipine: substrate CYP3A4 (increase cyclosporine level)
  • Diltiazem: major substrate CYP3A4 (increase cyclosporine level)

  • Start at lower dose and increase gradually 
  • If cardiovascular diseases, consult family doctor / internal medicine or cardiologist to evaluate risks / benefits
  • Assess for drug-drug interactions
  • Assess for other anti-hypertensive agents (may increase risk of hypotension)
  • If side effects, decrease dose